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Allergies

The formulation and composition of Prednisolone are produced by many pharmaceutical companies, with the same dosage of the active substance, the preparations can differ in appearance, in the content of the auxiliary components and in the package.

Inhibiting the enzyme phospholipase A2, lipocortin inhibits the release of arachidonic acid, as well as the synthesis of prostaglandins and leukotrienes, which contribute to inflammatory, allergic and other pathological processes.

Prednisolone inhibits pituitary release of β-lipotropin, but the concentration of circulating β-endorphin does not decrease, it inhibits the secretion of thyrotropin-releasing hormone (TSH) and FSH (follicle-stimulating hormone), increases the excitability of the CNS (central nervous system), reduces the number of lymphocytes, eosinophils, increases the number of blood cells , stimulating the production of erythropoietins.

Pharmacological action of the drug in systemic use (tablets, solution for injections in ampoules Prednisolone):
▶protein metabolism: reduces the content of globulin in the plasma, increasing the synthesis in the liver and kidneys of albumins (with an increase in the ratio of albumin / globulin);
▶increases protein catabolism in muscle tissue;
▶lipid exchange: stimulates the synthesis of triglycerides and higher fatty acids;
▶redistributes fatty deposits, moving them mainly to the face, shoulder girdle, abdomen;
▶can lead to the development of hypercholesterolemia;
▶carbohydrate metabolism: enhances absorption from the digestive tract (gastrointestinal tract) carbohydrates;
▶increases the intake of glucose from the liver into the bloodstream by increasing the activity of glucose-6-phosphatase;
▶increases the activity of FEPKK (phosphoenolpyruvate carboxylase) and improves the synthesis of aminotransferases by activating gluconeogenesis;
▶can lead to the development of hyperglycemia;
▶water-electrolyte balance: delays sodium and water in the body;
▶stimulates the excretion of potassium due to the increase in mineralocorticoid activity;
▶reduces absorption of calcium in the digestive tract, flushes calcium from bone tissue, increasing its excretion in the urine;
▶inflammatory processes: inhibits the release of inflammatory mediators by eosinophils and mast cells;
▶induces the formation of lipocortin and the reduction in the number of mast cells producing hyaluronic acid;
▶reduces the permeability of capillaries;
▶stabilizes cell membranes and membranes of organelles (especially lysosomal);
▶allergic reactions: suppresses the synthesis and secretion of mediators of allergy, inhibits the release of histamine and other bioactive substances from sensitized mast cells and basophils;
▶reduces the number of circulating basophils; suppresses the development of lymphoid and connective tissues;
▶reduces the number of mast cells, T- and B-lymphocytes;
▶oppresses the sensitivity of effector cells to mediators of allergy;
▶inhibits antibody formation;
▶changes the immune response of the body;
▶obstructive diseases of the respiratory tract: inhibits inflammatory processes, prevents or depresses the development of edema of the mucous membranes, inhibits eosinophilic infiltration of the submucosal layer of the bronchi epithelium and the deposition of immune complexes circulating in the mucous membrane of the bronchi;
▶stops erosion and desquamation of the mucosa;
▶increases the sensitivity of β-adrenoreceptors to endogenous catecholamines and exogenous sympathomimetics in bronchi of small and medium caliber;
▶reduces the viscosity of mucus by suppressing or reducing its production;
▶shock states, intoxications: increases blood pressure (arterial pressure) due to the increase in the concentration of circulating catecholamines and the restoration of receptor responsiveness to them, as well as the narrowing of the lumen of blood vessels;
▶reduces the permeability of the vascular wall, has a membrane-protective effect, activates liver enzymes involved in metabolic processes of endo- and xenobiotics;
▶immunosuppressive (immunosuppressive) therapy: inhibits the proliferation of lymphocytes (especially T-lymphocytes), suppresses B-cell migration and T-B and B-lymphocyte binding, inhibits the release of cytokines (interleukin-1 and -2, gamma-interferon) from lymphocytes and macrophages , reducing the formation of antibodies;
▶during the inflammatory process inhibits connective tissue reactions and reduces the possibility of keloid tissue formation.

Pharmacokinetics
Absorption of Prednisolone is high, with oral intake of tablets Prednazolone, the maximum concentration in the blood is reached after 1-1.5 hours. Up to 90% of the substance in the plasma binds to proteins: albumins and cortisol-binding globulin – transcortin.
The drug is metabolized in the kidneys, liver, bronchi, and small intestine. In oxidized forms, the substance is glucuronized or sulfated. Its metabolites are inactive.
T½ (half-life) is 2-4 hours, Prednisolone is excreted with bile and urine by glomerular filtration, 80-90% is reabsorbed by tubules, up to 20% is excreted unchanged by the kidneys. After intravenous injection of T1 Prednisolone from the plasma is 2-3 hours.
With topical application after absorption to the general bloodstream from the skin surface and from the conjunctival cavity, Prednisolone binds to plasma proteins and is metabolized predominantly in the liver; is excreted in the urine unchanged ≥ 20%, T½ is about 3 hours.

OintmentPrednisolone ointment is used in the complex treatment of such inflammatory and allergic skin diseases of non-microbial etiology as eczema, neurodermatitis, psoriasis, lupus erythematosus, erythroderma, as well as allergic, seborrheic and contact dermatitis.

Eye Drops
↗blunt and sharp eye trauma;
↗keratitis (under the condition of complete intact epithelium of the cornea);
↗allergic blepharoconjunctivitis in chronic course;
↗uveitis of the anterior segment of the eye, sclerites, episcleritis;
↗postoperative period (in case of prolonged symptoms of irritation of the eyeball).

Contraindications
With short-term systemic use of Prednisolone according to vital indications, the only contraindication for its use is an increased individual sensitivity to the acting or auxiliary components.

Prednisolone ointment is contraindicated in bacterial, viral, fungal skin lesions, tuberculosis, syphilis, skin tumors, vulgar acne, rosacea, skin post-vaccination reactions, open wounds, trophic ulcers, in children under 1 year and with increased individual sensitivity to its components. With caution, ointment is used in pregnancy and lactation.

Contraindications to the use of eye drops Prednisolone:
↘increased intraocular pressure;
↘dendritic keratitis caused by Herpes zoster, chicken pox, other viral diseases of the cornea and conjunctiva;
↘Fungal, mycobacterial, acute purulent eye diseases;
↘corneal epitheliopathy;
↘hypersensitivity to the components of the drug.

Instructions for use Prednisolone: method and dosage
The dose of Prednisolone and the duration of treatment are selected by the doctor individually, depending on the indications and severity of the disease.

Pills
Tablets Prednisolone is taken orally, washed down with a small amount of liquid, in the morning (from 6 to 8 o’clock in the morning) at breakfast or immediately after it. Usually take a daily dose daily, or a double dose – every other day. The high daily dose is divided into 2-4 admission, most of it is taken in the morning.

In acute conditions and as a substitute treatment for adults, it is recommended to start with a dose of 20-30 mg / day; maintenance therapy is carried out at a dose of 5-10 mg / day, some diseases (for example, nephrotic syndrome, individual rheumatic diseases) require higher doses.

If there is a history of psychosis, high-dose therapy is administered under the strict supervision of a specialist. When appointing, the daily secretory rhythm of the GCS is taken into account: in the mornings, the whole dose is taken at a time or a large part of it.

InjectionPrednisolone in the form of a solution is administered intravenously, usually the first injection is done in struyno, and repeated injections are drip. If intravenous administration is impossible for any reason, the solution in the same doses is administered intramuscularly.

Application according to indications:
➲acute adrenal insufficiency: single dose – 100-200 mg; daily – 300-400 mg;
➲severe allergic reactions: daily dose – 100-200 mg, duration of the course – 3-16 days; bronchial asthma: course dose – 75-675 mg, duration of the course – 3-16 days;
➲in severe cases, it is possible to increase the exchange rate to 1400 mg and above;
➲asthmatic status: the starting daily dose is 500-1200 mg followed by a gradual decrease to 300 mg and the transition to maintenance doses;
➲thyrotoxic crisis: 100 mg 2-3 times a day, if necessary daily dose can be increased to 1000 mg;
➲the duration of the course depends on the therapeutic effect and is usually at least 6 days;
➲shock, resistant to standard therapy: the initial dose, as a rule, injected, then transferred to drip infusions;
➲if the blood pressure does not rise within 10-20 minutes, repeat the jet injection. After excretion from the state of shock, drip administration is continued until BP stabilizes. Single dose – 50-150 mg (in severe cases, increase to 400 mg);
➲repeated administration is carried out after 3-4 hours;
➲daily dose varies from 300 to 1200 mg with a further gradual decrease;
➲acute hepatic / renal failure (acute poisoning, postoperative or postpartum periods, etc.): daily dose – 25-75 mg; according to the indications, it is possible to increase it to 300-1500 mg or more;
➲rheumatoid arthritis and SLE: 75-125 mg / day administered for no more than 7-10 days in addition to the systemic intake of Prednisolone;
➲acute hepatitis: daily dose – 75-100 mg, duration of the course – 7-10 days;
➲poisoning with cauterizing liquids, burns of the upper respiratory tract and digestive tract: a daily dose of 75 to 400 mg, depending on the severity of the condition, the duration of the course is 3-18 days.

Do not suddenly stop prolonged therapy with Prednisolone. After relief of acute conditions, they switch to oral administration of the drug in the form of tablets with a gradual dose reduction.

Recommended dosage for children: from 2 to 12 months – at the rate of 2-3 mg / kg; from 1 to 14 years – 1-2 mg / kg; the solution is administered intramuscularly, and when such administration is not possible – intravenously slowly (about 3 minutes). If necessary, you can re-enter the same dose after 20-30 minutes.

Ointment
Ointment is applied externally, applying a thin layer on the affected skin.

To enhance the effect in limited areas, occlusive dressings can be used.
Recommended dosing: apply ointment 1-3 times a day, the duration of the course is, as a rule, 6-14 days; In the process of aftercare, the use of the drug once a day is allowed.

In order to prevent relapse and in the treatment of chronic diseases, the use of ointment continues for some time after the complete disappearance of all symptoms, but no longer than 14 days.
Areas with more dense skin (palms, feet, elbows), as well as places where the ointment is easily washed, can be lubricated more often.

Eye Drops
The drug is buried in the conjunctival sac. The duration of the course is determined by the attending physician.
Standard therapeutic dosing regimen Prednisolone: 1-2 drops 2-4 times a day.

In order to relieve inflammatory symptoms due to trauma to the eyeball, instillation of Prednisolone is recommended to be performed once a day.

Ointment
Possible side effects due to the use of ointment Prednisolone: ​​steroid acne, purpura, telangiectasia, burning, itching, irritation and dry skin.

Prolonged use and / or application of ointment on large surfaces can cause the development of hypercorticism due to the resorptive effect of Prednisolone. In such cases, the drug should be discontinued and consult a specialist.
If these side effects are aggravated or any other reactions not indicated in this manual occur, you should inform your doctor about them.

Eye Drops
After instillation of Prednisolone, a transient burning sensation is possible.
The result of prolonged use may be an increase in intraocular pressure, and therefore preparations containing GCS, use no more than 10 days and under regular control of intraocular pressure.

Continuous use of the eye suspension for 3 months or more can cause the development of a posterolateral cataract.

Overdose
A sign of systemic overdose of Prednisolone is an increase in dose-dependent side effects. It is recommended to carry out symptomatic treatment with a gradual dose reduction, if necessary until the drug is discontinued.
Overdosing with topical application (ointment, eye suspension) can cause local side effects in the form of allergic reactions, the occurrence of which requires immediate withdrawal of the drug.

Special instructions
Before the beginning of therapy, to identify possible contraindications, it is necessary to conduct a clinical examination of the patient, including lung fluoroscopy, examination of the gastrointestinal tract, cardiovascular system, vision and urinary system.

Before the start of treatment and during steroid therapy it is required to regularly monitor general blood counts, the concentration of electrolytes in plasma, the glucose content in urine and blood. Do not vaccinate during the use of GCS, especially in high doses, as its effectiveness will be reduced.

With tuberculosis Prednisolone is prescribed only in combination with anti-tuberculosis drugs. Systemic administration of medium and high doses of the drug may cause an increase in blood pressure. The use of Prednisolone in intercurrent infections associated with septic conditions should be carried out with the support of antibiotic therapy.

Long-term treatment with GCS requires the administration of potassium preparations to avoid hypokalemia. With chronic adrenocortical insufficiency (Addison’s disease) Prednisolone is contraindicated to be taken concomitantly with barbiturates in connection with the danger of the addisonic crisis. In the event of a sudden discontinuation of the drug, especially with high-dose therapy, there is a syndrome of cancellation of the SCS, accompanied by a worsening of appetite, nausea, retardation, generalized musculoskeletal pain, asthenia.

Reduce the likelihood of adrenal insufficiency and associated complications can be, by gradual abolition of Prednisolone. In connection with the fact that adrenal insufficiency after drug cancellation can last for months, any stressful situation in this period requires the resumption of hormone therapy.

The presence of hypothyroidism and / or cirrhosis in the patient may exacerbate the effect of GCS. Patients should be warned in advance about the need for them and their environment to avoid contact with infected measles, herpes and chicken pox. With the current systemic treatment of GCS, or if they have been used in the next 3 months, patients who do not receive vaccination require specific immunoglobulins.

In the case of replacement therapy of adrenal insufficiency due to a weak mineralocorticoid effect, Prednisolone is recommended to be used in combination with mineralocorticoids. When diabetes is required to monitor blood glucose and, if necessary, correction of the dosing regimen. Periodic x-ray control of the osteoarticular system is recommended (photos of hands, spine). In patients with infectious diseases of the kidneys and urinary tract in the latent course, Prednisolone can cause leukocyturia, clinically significant for diagnosis.

GCS increases the metabolites of 11- and 17-oxyketocorticosteroids. Like other local GCS, Prednisolone ointment can not be applied to the skin around the eyes because of the risk of developing glaucoma / cataracts, as well as open wound surfaces. In case of complication of the disease by the development of a secondary fungal or bacterial infection, a specific antibacterial / antimycotic drug should be added to the therapy with Prednisolone.

Drops Prednisolone is not recommended with contact lenses, you should remove the lenses before instillation and wear again not earlier than 15 minutes after the procedure. Long-term use of drops can increase intraocular pressure, so if used for 2 weeks or more, regular monitoring of intraocular pressure is required. SCS therapy can mask the symptoms of a current bacterial / fungal infection, the presence of which is an indication for the use of Prednisolone as part of a complex therapy with antibiotics for topical use.

Influence on ability to manage motor transport and complex mechanisms
According to the instructions, Prednisolone used systemically can cause dizziness and other side reactions that can affect coordination of movements, reaction speed and concentration of attention, so it is not recommended to drive vehicles and maintain mechanical equipment during therapy.

After instillation of Prednisolone suspension, lacrimation is possible, and therefore it is not necessary to carry out the procedure immediately before carrying out potentially hazardous activities. Data on the effects of Prednisolone in the form of an ointment on the ability to drive vehicles and complex mechanisms is not available.

Application in pregnancy and lactation
The use of Prednisolone systemically and topically, in the form of eye drops during pregnancy is possible according to vital indications in case of justifiable excess of the intended benefit for the mother over the potential risk to the fetus.

Long-term systemic therapy of GCS in pregnant women does not exclude the possibility of impaired fetal growth. The use of Prednisolone in the third trimester increases the risk of atrophy of the adrenal cortex of the fetus, so that a newborn may require replacement therapy. Apply Prednisolone topically as short as possible, the ointment should be applied to small areas of the skin surface.

GCS is excreted in breast milk, so when used during breastfeeding it is necessary to take precautions, in particular, not apply ointment on the breast skin shortly before feeding. If you need systemic use of the drug during lactation, or apply to the skin ointment Prednisolone in large doses and / or for an extended period, breast-feeding should be interrupted for the duration of therapy.

Application in childhood
In pediatrics, GCS is used only under absolute indications, under the careful supervision of a physician, since they are capable of causing a slowdown in growth in children and adolescents.

Usually, the risk of developing such side effects helps to avoid or minimize the use of Prednisolone every other day. Children who are in the process of treatment in contact with infected measles or chickenpox require specific immunoglobulins for prevention.

The ratio of the area to the body weight in children is greater than in adults, so they are more at risk of suppressing the function of the hypothalamic-pituitary-adrenal system and the development of hypercortisy syndrome due to the use of any GCS for local use. In infants, diapers, diapers and skin folds can have an effect similar to occlusive dressing, thereby increasing systemic resorption of Prednisolone.

In childhood and adolescence, Prednisolone should be applied at the lowest effective dose, the maximum possible short course, and necessarily under the supervision of a specialist.

For violations of kidney function Tablets and solutionPrednisolone is not prescribed for patients with severe renal failure and with nephrourolythiasis.

For violations of liver function
Tablets and solution Prednisolone is not prescribed for patients with severe hepatic insufficiency.

Application in the elderly
With the use of GCS in the elderly, the incidence of adverse reactions increases.

Drug Interactions
In connection with high pharmacological activity, Prednisolone, like other GCS, can weaken or enhance the action of many drugs / drugs.

If you need to use a solution, tablets or eye drops of Prednisolone in combination with other drugs, the attending physician should consider and take into account their possible interaction. There is no data on the drug interaction of the ointment.

In connection with the possible pharmaceutical incompatibility of the solution of Prednisolonewith other drugs administered intravenously, it is recommended to administer it separately: bolus, or through another dropper. Mixing of solutions of Prednisolone and heparin occurs with the formation of a precipitate.

Terms and conditions of storage
Store in a place protected from light and out of reach of children, at a temperature of: tablets – up to 25 ° C, ointment, injection solution – up to 15 ° C, do not freeze the solution; eye drops – 15-25 ° C, open the bottle for 4 weeks.
The shelf life depends on the manufacturer (see the packaging).

Reviews of Prednisolone
According to reviews, Prednisolone in systemic administration (tablets, injections) is quite effective, but patients complain of a large number of side effects. It is difficult to stop receiving after a long course of therapy because of withdrawal syndrome, so you should strictly follow the requirement for a gradual cessation of treatment.
There are complaints about painful injections. It is noted that in emergency cases, parenteral administration of Prednisolone quickly suppresses critical conditions and can save life. Application of the drug in topical forms (ointment, eye drops) practically does not cause side effects, and reviews about them are mostly positive.